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Catalog No.
Product Name
Application
Product Information
Citations
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PC Inhibitor
Anemoside A3-methyl 6-aminohexanoate is a potent pyruvate carboxylase (PC) inhibitor, exhibiting a Kd value of 10.1 μM against human PC. This compound influences cellular pathways through the PC/NF-κB/NLRP3 inflammasome axis, demonstrating significant efficacy in alleviating symptoms of DSS-induced colitis in murine models. Anemoside A3-methyl 6-aminohexanoate serves as a useful tool in colitis-related research and studies focusing on the modulation of inflammatory pathways. -
NLRP3 Inhibitor
Yadanzigan is a potent NLRP3 inhibitor that exerts its anti-inflammatory effects by inhibiting the NF-κB signaling pathway and reducing Reactive Oxygen Species production. This compound has been shown to mitigate LPS-induced acute lung injury (ALI) in murine models, highlighting its potential for research in inflammation-related conditions. Its mechanism of action positions Yadanzigan as a valuable tool for studying NLRP3-related pathways and their roles in various pathological processes. -
Sodium Channel Inhibitor
Articaine is a selective inhibitor of voltage-gated sodium channels, including rNav1.4, hNav1.7, and rNav1.8, demonstrating an IC50 of 15.8 μM for open-state Na+ channels. It effectively blocks Na+ influx, leading to local anesthetic effects and interruption of nerve impulse conduction. Additionally, Articaine exhibits anti-inflammatory properties by inhibiting NF-κB activation and the NLRP3 inflammasome pathway. This compound is valuable for research in dental anesthesia and inflammatory-related conditions, such as acute kidney injury. -
NLRP3 Inhibitor
NLRP3-IN-69 is a selective inhibitor of the NLRP3 inflammasome, targeting the activation of NF-κB p65. This compound effectively reduces LPS-induced overexpression of pro-inflammatory cytokines including IL-1β, as well as iNOS and COX-2, while inhibiting nitric oxide generation with an IC50 of 5.66 μM. NLRP3-IN-69 serves as a valuable tool in research focused on inflammatory diseases and the modulation of the immune response. -
COX-2/NLRP3 Inhibitor
COX-2/NLRP3-IN-1 is a selective inhibitor targeting both COX-2 and the NLRP3 inflammasome, with an IC50 of 1.53 μM for COX-2. This compound exhibits notable anti-inflammatory properties by disrupting the NF-κB/NLRP3 signaling pathway, making it a valuable tool for research into inflammatory diseases. It is suitable for studying the roles of COX-2 and NLRP3 in various biological processes and therapeutic interventions. -
NF-κB Inhibitor
1-Caffeoylquinic acid is a potent inhibitor of NF-κB, demonstrating a significant binding affinity to the RH domain of p105 with a Ki value of 0.007 μM. This compound exhibits notable anti-oxidative stress properties and serves as an inhibitor for the PD-1/PD-L1 pathway. Its biological activities make it valuable for research applications in inflammation, immunity, and cancer studies. -
CHI3L1 Inhibitor
K284-6111 is a potent inhibitor of CHI3L1, demonstrating high affinity and oral bioavailability. It effectively suppresses CHI3L1 expression and disrupts key signaling pathways, including ERK and NF-κB, leading to reduced nuclear translocation of p50 and p65 as well as decreased phosphorylation of IκB. K284-6111 shows promise in alleviating memory dysfunction associated with Alzheimer's disease by mitigating amyloidogenesis and neuroinflammation. Additionally, it exhibits therapeutic potential in reducing atopic-like skin inflammation and protecting against LPS-induced liver injury. This compound is suitable for research into neurodegenerative diseases and inflammatory conditions. -
NF-κB Inhibitor
Valencene is a sesquiterpene that functions as an NF-κB inhibitor. It exhibits significant anti-inflammatory, antiallergic, and antioxidant activities by inhibiting the expression of Th2 chemokines and proinflammatory cytokines. In LPS-stimulated RAW 264.7 cells, Valencene effectively reduces the production of IL-1β and IL-6. Additionally, Valencene has demonstrated potential in alleviating symptoms of atopic dermatitis and restoring filaggrin expression in a DNCB-sensitized mouse model. -
NF-κB Inhibitor
Dimethyl diacetyl cystinate (DACDM) is a potent NF-κB inhibitor that modulates inflammation by shifting the intracellular redox balance towards an oxidized state. This compound increases the levels of oxidized glutathione (GSSG) and competes with activated NF-κB for binding sites on DNA, thus inhibiting the production of pro-inflammatory cytokines such as IL-1κ. DACDM is a valuable reagent for studies related to UVB-induced skin inflammation and various oxidative stress-related diseases. -
Akr1B1 Inhibitor
β-Glucogallin is a selective inhibitor of aldose reductase (AKR1B1), exhibiting an IC50 value of 58 μM with glyceraldehyde as the substrate. This compound displays significant antioxidant properties, reducing reactive oxygen species (ROS) and influencing key pathways involving PDGF, RAGE, and NF-κB. Additionally, β-Glucogallin enhances superoxide dismutase (SOD) activity and demonstrates hepatoprotective effects. Its biological activity makes it a valuable tool for research in retinal studies and related fields. -
HIPK2 Inhibitor
XRF-1021 is an orally active inhibitor of Homer-interacting protein kinase 2 (HIPK2), with an IC50 value of 0.18 μM. It effectively decreases the expression of fibrotic markers such as Fibronectin, Collagen I, and α-SMA in TGF-β1 stimulated renal cell lines, including NRK-49F and HK-2. XRF-1021 further inhibits key signaling pathways including TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch. This compound demonstrates potential in reducing renal injury and fibrosis in vivo, making it a valuable tool for research on chronic kidney disease. -
Toll-like Receptor (TLR) Inhibitor
Okanin is a potent Toll-like Receptor (TLR) inhibitor derived from the flowering plant Coreopsis tinctoria. It exhibits significant biological activity by attenuating lipopolysaccharide (LPS)-induced microglial activation via the inhibition of the TLR4/NF-κB signaling pathway. This compound is useful for research applications focusing on neuroinflammation and the modulation of immune responses in microglial cells. -
GPR75 Inhibitor
(Rac)-AAA is a potent inhibitor of GPR75, targeting the receptor to modulate key signaling pathways. This compound effectively blocks the downregulation of GPR75 expression induced by 20-HETE, leading to the inhibition of downstream pathways such as EGFR, AKT, NF-κB, and FAK. (Rac)-AAA also reverses 20-HETE-mediated epithelial-mesenchymal transition, characterized by the downregulation of vimentin and upregulation of E-Cadherin, while reducing MMP-2 activity and cancer cell migration. Additionally, it mitigates the upregulation of HIC-5 and affects the localization of PKC-α and phosphorylated AKT, making (Rac)-AAA a significant tool in the study of castration-resistant prostate cancer. -
RPTPβ/ζ Inhibitor
MY10 is a potent inhibitor of receptor protein tyrosine phosphatase β/ζ (RPTPβ/ζ) that exhibits oral bioactivity. It has been shown to reduce NF-κB p65 expression and activate c-Met tyrosine phosphorylation. Additionally, MY10 prevents the alcohol-induced downregulation of Ptprz1 and Alk expression, while attenuating binge-like ethanol consumption and associated rewards. This compound is valuable for investigating neurological and vascular diseases. -
COX-1/cAMP Phosphodiesterase Inhibitor
Triflusal is a dual inhibitor of Cyclooxygenase-1 (COX-1) and cAMP phosphodiesterase, which penetrates the blood-brain barrier. It effectively inhibits platelet aggregation, nuclear factor kappa B (NF-κB) activation, inducible nitric oxide synthase (iNOS) activity, and prostaglandin synthesis in ischemic tissues. Additionally, Triflusal enhances neutrophil nitric oxide production, endothelial nitric oxide synthase (eNOS) expression, and constitutive nitric oxide synthase (cNOS) activity. This compound is valuable for investigating thromboembolic and ischemic diseases of the cardiovascular and cerebrovascular systems, as well as Alzheimer's disease pathology. -
COX Inhibitor
Pentagamavunon-1 (PGV-1) is a COX-2 inhibitor that modulates multiple molecular pathways to induce apoptosis. This Curcumin analog exhibits notable oral bioactivity and suppresses key angiogenic factors, including vascular endothelial growth factor (VEGF). Additionally, PGV-1 inhibits NF-κB activation, highlighting its potential in cancer research and therapeutic applications targeting inflammation and tumor progression. -
NF-κB/MAPK/FAK/Akt Inhibitor
Ephemeranthol A is an inhibitor of NF-κB, MAPK, FAK, and Akt signaling pathways. This phenanthrene compound demonstrates notable anti-inflammatory effects through the inhibition of NF-κB and MAPK pathways in macrophages. Additionally, Ephemeranthol A induces apoptosis and inhibits metastasis in non-small cell lung cancer by suppressing FAK/Akt signaling and epithelial-mesenchymal transition (EMT) processes. It is applicable for research into acute and chronic inflammatory diseases as well as non-small cell lung cancer. -
NF-κB p65 Inhibitor, Apoptosis Inducer
N-Desmethyldauricine is an inhibitor of NF-κB p65 with significant apoptotic effects. It effectively reduces p65 protein expression, induces apoptosis, and arrests the cell cycle at the G0/G1 phase. Additionally, N-Desmethyldauricine attenuates intercellular adhesion and inhibits the growth of 3D spheroids derived from triple-negative breast cancer. This compound is useful for research involving triple-negative breast cancer dynamics and therapeutic strategies. -
NF-κB Inhibitor
15-Deoxy-Δ12,14-prostaglandin A1 is a potent inhibitor of NF-κB signaling, functioning through the modulation of inflammatory pathways. It has been shown to induce apoptosis and effectively inhibit TNF-α-induced upregulation of adhesion molecules on endothelial cells, thereby preventing monocyte arrest. This compound is valuable for research in inflammation, cardiovascular diseases, and apoptosis studies. -
NF-κB Inhibitor
Declopramide is a potent NF-κB inhibitor that exerts antitumor effects by inducing apoptosis in cancer cells. It has demonstrated efficacy in inhibiting the proliferation of HL60 and K562 cell lines, as well as reducing tumor growth in a mouse model of human brain astrocytoma (T24). Additionally, Declopramide functions as a chemosensitizer, making it a valuable tool for investigating therapeutic strategies in cancer research. -
TLR4/NF-κB Inhibitor
TLR4/NF-κB-IN-1 is a selective inhibitor of the TLR4/NF-κB signaling pathway, demonstrating significant anti-inflammatory properties. This compound exhibits the ability to penetrate the blood-brain barrier, making it suitable for studies involving neuroinflammation. In murine models, TLR4/NF-κB-IN-1 effectively reduces acute neuroinflammation induced by lipopolysaccharides (LPS) while downregulating the expression of TLR4, phosphorylated NF-κB, and phosphorylated IκB-α proteins, providing a valuable tool for researching neuroinflammatory processes and their therapeutic modulation. -
TLR4/MyD88/NF-κB Inhibitor
SjDX5-271 is a small peptide inhibitor targeting the TLR4/MyD88/NF-κB signaling pathway. It is known to induce cell polarization and mitigate hepatic inflammation, demonstrating protective effects against liver ischemia-reperfusion injury in mouse models. This compound is valuable for research in immunology and liver-related inflammation studies. -
TLR7/TLR9 Inhibitor
ODN 24888 is a guanine-modified inhibitory oligonucleotide (INH-ODN) that specifically targets TLR7 and TLR9 signaling pathways. It effectively inhibits interferon-alpha (IFN-α) secretion and NF-κB activation, while also reducing interleukin-6 (IL-6) release. ODN 24888 is valuable for studying immune and inflammatory responses and can be utilized as a vaccine adjuvant in various research applications. -
TLR Inhibitor
TIC10g is a dual inhibitor of toll-like receptors 7 and 9 (TLR7 and TLR9). It effectively decreases TNF-α release in mouse macrophages and human B lymphocytes, with IC50 values of 14.5 μM and 6.5 μM for TLR7, and 7.69 μM and 11.5 μM for TLR9, respectively. TIC10g also inhibits the activation of NF-κB and MAPK pathways, demonstrating potential as an anti-inflammatory agent in conditions such as systemic lupus erythematosus and rheumatoid arthritis. -
TLR4 Signaling Inhibitor
NCI126224 is a TLR4 signaling inhibitor that modulates immune responses by suppressing lipopolysaccharide (LPS)-induced production of key inflammatory mediators, including NF-κB, TNF-α, IL-1β, and nitric oxide. This compound demonstrates biological activity in the low nanomolar to low micromolar range, making it a valuable tool for research into inflammatory diseases and their mechanisms. Its ability to interfere with TLR4 signaling pathways positions NCI126224 as a significant reagent for exploring potential therapeutic strategies in inflammation-related studies. -
TLR4/NF-kB/MAPK Inhibitor
TLR4/NF-κB/MAPK-IN-1 is an inhibitor targeting the TLR4/NF-κB/MAPK signaling pathways. It exhibits significant anti-neuroinflammatory activity by suppressing the activation of these pathways, leading to reduced inflammatory responses. This compound is particularly useful for research applications focusing on neuroinflammation and related neurodegenerative diseases. -
TLR4/NF-κB Inhibitor
Ligusticum cycloprolactam is a potent TLR4/NF-κB inhibitor with significant anti-inflammatory properties. It has been shown to alleviate renal injury by effectively disrupting the TLR4/NF-κB signaling pathway in both in vivo and in vitro models. In studies, Ligusticum cycloprolactam reduces serum uric acid levels, diminishes tubular damage, and decreases inflammatory infiltration and interstitial collagen deposition, leading to improved renal function. This compound serves as a valuable reagent for research into hyperuricemic nephropathy. -
NF-κB Inhibitor
NF-κB-IN-14 is an NF-κB inhibitor that effectively modulates inflammatory responses by significantly inhibiting nitric oxide production in LPS-stimulated macrophages, with an IC50 of 6.4 μM. This compound disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway. Additionally, NF-κB-IN-14 has demonstrated efficacy in reducing ear edema and inflammation in a mouse model of atopic dermatitis, highlighting its potential utility in inflammatory research. -
MyD88 Inhibitor
LM9 is a selective inhibitor of MyD88, a key adaptor protein in the Toll-like receptor (TLR) signaling pathway. By blocking the binding of TLR4 to MyD88, LM9 disrupts MyD88 homodimer formation and subsequent activation of the NF-κB signaling pathway. This compound demonstrates significant anti-inflammatory effects, mitigating atherosclerosis and fibrosis in models of obesity-induced cardiomyopathy. LM9 is valuable for research focused on understanding the mechanisms of inflammation, fibrosis, and cardiovascular diseases. -
TLR4/JNK/NF-κB Inhibitor
TLR4-IN-2 is an inhibitor targeting TLR4, JNK, and NF-κB pathways. It demonstrates anti-inflammatory properties by reducing nitric oxide production in LPS-stimulated RAW264.7 cells, with an IC50 of 23.2 µM. By inhibiting TLR4 expression and diminishing JNK phosphorylation, TLR4-IN-2 effectively suppresses NF-κB activation and the transcription of inflammation-related genes, leading to lower levels of iNOS, COX-2, and various inflammatory mediators. This compound shows potential for investigating therapeutic strategies in inflammatory diseases such as rheumatoid arthritis and other inflammatory disorders. -
NF-κB Inhibitor
Ergolide is a selective NF-κB/p65 and NLRP3 inhibitor that effectively disrupts the NF-κB signaling pathway and inhibits the nuclear translocation of p65. By irreversibly binding to the NACHT domain of NLRP3, Ergolie suppresses inflammasome assembly, significantly reducing the production of inflammatory mediators such as NO and PGE2. This compound promotes apoptosis in cancer cells, induces autophagy, and generates reactive oxygen species (ROS). Ergolide also enhances the therapeutic efficacy of vincristine and has been shown to alleviate acute lung injury in models of sepsis and inflammation, contributing to research in metastatic uveal melanoma, neurodegenerative diseases, and acute lymphoblastic leukemia. - Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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NF-κB inhibitor
Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B is also a regulator of skeletal muscle mass. -
NF-κB inhibitor
Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. -
NF-κB inhibitor
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122?±?30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells. -
NF-κB inhibitor
Edasalonexent (CAT-1004) is an orally bioavailable NF-κB inhibitor. -
NF-κB inhibitor
DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect. -
NF-κB inhibitor
DHMEQ racemate is a NF-κB inhibitor. DHMEQ racemate is less active than (-)-DHMEQ. -
glutamate decarboxylase inhibitor
Chelidonic acid is a glutamate decarboxylase inhibitor, with a Ki of 1.2 μM. -
HMGB1 release inhibitor
Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent. -
NF-κB Inhibitor
Micheliolide is a sesquiterpene lactone that functions as an NF-κB inhibitor. It exhibits significant anti-cancer and anti-inflammatory properties by attenuating high glucose-induced NF-κB activation and reducing the expression of inflammatory mediators such as MCP-1, TGF-β1, and FN in mouse mesangial cells. Additionally, Micheliolide inhibits LPS-induced NF-κB activation and the PI3K/Akt/p70S6K pathways, making it a valuable tool for studying inflammatory disease models, including colitis-associated cancer and rheumatic arthritis. -
NF-κB Inhibitor
Aristolochic acid A is a potent NF-κB inhibitor derived from the plant extracts of Aristolochia and Asarum species. This compound effectively diminishes the activities of activator protein 1 (AP-1) and NF-κB, making it a valuable tool for studying signaling pathways related to inflammation and cancer. Additionally, Aristolochic acid A has been shown to downregulate BLCAP gene expression in human cell lines, highlighting its potential for investigating gene regulation mechanisms. -
STAT3/NF-κB Inhibitor
Triacetylresveratrol is an acetylated analog of Resveratrol that functions as an inhibitor of STAT3 and NF-κB signaling pathways. It effectively reduces the phosphorylation levels of STAT3 and NF-κB in a dose- and time-dependent manner in PANC-1 and BxPC-3 cancer cell lines. Its promising anticancer activity makes it a valuable tool for research in cancer biology and therapeutic development. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
TNF Receptor Inhibitor
Muscone, a TNF receptor inhibitor, is derived from the traditional Chinese medicine musk. It effectively inhibits NF-κB signaling and NLRP3 inflammasome activation, resulting in a significant reduction of inflammatory cytokines such as IL-1β, TNF-α, and IL-6. This compound is valuable in research focused on inflammation, cardiac function restoration, and improving survival rates in various pathological conditions. -
NF-κB Inhibitor
Sciadopitysin is a biflavonoid that serves as a potent NF-κB inhibitor. Its primary mechanism involves the inhibition of RANKL-induced osteoclastogenesis, contributing to the prevention of bone loss. By suppressing NF-κB activation and lowering the expression levels of c-Fos and NFATc1, Sciadopitysin demonstrates significant potential for research applications focused on bone metabolism and related disorders. -
Bacterial Inhibitor
Ceftiofur is a cell wall synthesis inhibitor targeting bacterial penicillin-binding proteins (PBPs). It demonstrates bactericidal activity by interfering with the peptidoglycan synthesis in bacterial cell walls, resulting in cell lysis. Additionally, Ceftiofur exhibits anti-inflammatory properties by inhibiting the activation of NF-κB and MAPKs, which decreases the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6. This makes Ceftiofur a valuable reagent in research investigating bacterial infections and inflammation processes. -
NF-κB Inhibitor
Cardamonin is a potent NF-κB inhibitor derived from cardamom. It exerts broad biological activity by targeting key signaling pathways, including mTOR, Akt, STAT3, Wnt/β-catenin, and COX-2. This compound has demonstrated significant anticancer, anti-inflammatory, antimicrobial, and antidiabetic properties, making it valuable for various research applications in cancer biology and inflammation studies.
